Structure, activity, regulation, and inhibitor discovery for a protein kinase associated with apoptosis and neuronal death
Death-associated protein kinase (DAPK) is a calmodulin-regulated serine/threonine protein kinase associated with neuronal cell death in animal models of disease. The recent determination of the 1.5Å crystal structure of the catalytic kinase domain of DAPK, the discovery of amino acid sequence motifs...
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| Veröffentlicht in: | Pharmacology & therapeutics (Oxford) 2002-02, Vol.93 (2), p.217-224 |
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| creator | Velentza, Anastasia V. Schumacher, Andrew M. Watterson, D.Martin |
| description | Death-associated protein kinase (DAPK) is a calmodulin-regulated serine/threonine protein kinase associated with neuronal cell death in animal models of disease. The recent determination of the 1.5Å crystal structure of the catalytic kinase domain of DAPK, the discovery of amino acid sequence motifs with sites that are preferentially phosphorylated by this kinase, and the development of a quantitative enzyme activity assay provide a firm foundation for future studies into its regulation, the identification of its physiological substrates, and discovery of inhibitors. We summarize the relevant background and ongoing investigations that will increase our understanding of the role and regulation of this prototype death-associated kinase. |
| doi_str_mv | 10.1016/S0163-7258(02)00190-0 |
| format | Article |
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We summarize the relevant background and ongoing investigations that will increase our understanding of the role and regulation of this prototype death-associated kinase.</description><subject>Animals</subject><subject>Apoptosis</subject><subject>Apoptosis - physiology</subject><subject>Apoptosis Regulatory Proteins</subject><subject>Calcium-Calmodulin-Dependent Protein Kinases - antagonists & inhibitors</subject><subject>Calcium-Calmodulin-Dependent Protein Kinases - metabolism</subject><subject>Calcium-Calmodulin-Dependent Protein Kinases - physiology</subject><subject>Calmodulin</subject><subject>Chemical genomics</subject><subject>Death-Associated Protein Kinases</subject><subject>Drug discovery</subject><subject>Kinase inhibitors</subject><subject>Protein kinase</subject><issn>0163-7258</issn><issn>1879-016X</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2002</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkFFvFCEQgEmjaa_Vn6DhydikqwMLt8tTYxrbmjTxoZr4RjiY9bB7cAX2zPnrpXeX-ujLEIZvZpiPkDcMPjBg84_3NbRNx2X_Hvg5AFPQwBGZsb5TTX378YLMnpETcprzLwAQAvgxOWGcKTZn7Yz8uS9psmVKeEGNLX7jy_aCJvw5jab4GGo2OOrD0i98iYk6n23cYNrSod4MXadY0Af64IPJSE3O0XpT0NHfviypWcd1idnnXZuAU4rBjNShKctX5OVgxoyvD-cZ-X79-dvVbXP39ebL1ae7xgrWlqbtDetE2zMuoFNi7qBnuJDY1eC4Yq5T_SCFkr0EIW0vBBollVFMGmMHbM_Iu33f-tfHCXPRq7oEjqMJGKesOw5cQisqKPegTTHnhINeJ78yaasZ6CfpeiddPxnVwPVOuoZa9_YwYFqs0P2rOliuwOUewLrmxmPS2XoMFp1PaIt20f9nxF-tkZLA</recordid><startdate>20020201</startdate><enddate>20020201</enddate><creator>Velentza, Anastasia V.</creator><creator>Schumacher, Andrew M.</creator><creator>Watterson, D.Martin</creator><general>Elsevier Inc</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>20020201</creationdate><title>Structure, activity, regulation, and inhibitor discovery for a protein kinase associated with apoptosis and neuronal death</title><author>Velentza, Anastasia V. ; Schumacher, Andrew M. ; Watterson, D.Martin</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c413t-38a1743812407946d081eb5e7eb5d291d798f549585045c844ea959a915aacfe3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2002</creationdate><topic>Animals</topic><topic>Apoptosis</topic><topic>Apoptosis - physiology</topic><topic>Apoptosis Regulatory Proteins</topic><topic>Calcium-Calmodulin-Dependent Protein Kinases - antagonists & inhibitors</topic><topic>Calcium-Calmodulin-Dependent Protein Kinases - metabolism</topic><topic>Calcium-Calmodulin-Dependent Protein Kinases - physiology</topic><topic>Calmodulin</topic><topic>Chemical genomics</topic><topic>Death-Associated Protein Kinases</topic><topic>Drug discovery</topic><topic>Kinase inhibitors</topic><topic>Protein kinase</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Velentza, Anastasia V.</creatorcontrib><creatorcontrib>Schumacher, Andrew M.</creatorcontrib><creatorcontrib>Watterson, D.Martin</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Pharmacology & therapeutics (Oxford)</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Velentza, Anastasia V.</au><au>Schumacher, Andrew M.</au><au>Watterson, D.Martin</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Structure, activity, regulation, and inhibitor discovery for a protein kinase associated with apoptosis and neuronal death</atitle><jtitle>Pharmacology & therapeutics (Oxford)</jtitle><addtitle>Pharmacol Ther</addtitle><date>2002-02-01</date><risdate>2002</risdate><volume>93</volume><issue>2</issue><spage>217</spage><epage>224</epage><pages>217-224</pages><issn>0163-7258</issn><eissn>1879-016X</eissn><abstract>Death-associated protein kinase (DAPK) is a calmodulin-regulated serine/threonine protein kinase associated with neuronal cell death in animal models of disease. 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| identifier | ISSN: 0163-7258 |
| ispartof | Pharmacology & therapeutics (Oxford), 2002-02, Vol.93 (2), p.217-224 |
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| language | eng |
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| source | MEDLINE; ScienceDirect Journals (5 years ago - present) |
| subjects | Animals Apoptosis Apoptosis - physiology Apoptosis Regulatory Proteins Calcium-Calmodulin-Dependent Protein Kinases - antagonists & inhibitors Calcium-Calmodulin-Dependent Protein Kinases - metabolism Calcium-Calmodulin-Dependent Protein Kinases - physiology Calmodulin Chemical genomics Death-Associated Protein Kinases Drug discovery Kinase inhibitors Protein kinase |
| title | Structure, activity, regulation, and inhibitor discovery for a protein kinase associated with apoptosis and neuronal death |
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